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| United States Patent |
5,059,606
|
|
Grollier
, et al.
|
October 22, 1991
|
Combination of pyrimidine derivatives and calcium antagonists to induce
and stimulate hair growth and reduce hair loss
Abstract
A combination intended to induce and stimulate hair growth and reduce hair
loss comprising a first component containing at least one calcium
antagonist in a physiologically acceptable medium and a second component
containing, in a physiologically acceptable medium, at least one
pyrimidine derivative having the formula:
##STR1##
In formula (I) R.sub.1 represents the group
##STR2##
in which R.sub.3 and R.sub.4 are independent of each other and represent
hydrogen, an alkyl, alkenyl, alkylaryl or cycloalkyl group, or R.sub.3 and
R.sub.4 form a heterocycle with the nitrogen atom joined thereto, and
represent an aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl,
hexahydroazepinyl, heptamethyleneimine,
octamethyleneimine, morpholine or 4-alkylpiperazidinyl group, the
heterocyclic groups further being substitutable at the carbon atoms by one
to three low alkyl, hydroxy or alkoxy groups. In formula (I) R.sub.2
represents a hydrogen atom, an alkyl, alkenyl, alkylalkoxy, cycloalkyl,
aryl, alkylaryl, arylalkyl, alkylarylalkyl, alkoxyarylalkyl or
haloarylalkyl group. The addition salts of physiologically acceptable
acids may also be employed. The first and second components may form part
of the same composition or may be used separately, either simultaneously
or in successive or separate stages.
| Inventors:
|
Grollier; Jean F. (Paris, FR);
Rosenbaum; Georges (Asnieres, FR)
|
| Assignee:
|
L'Oreal (Paris, FR)
|
| Appl. No.:
|
281273 |
| Filed:
|
December 8, 1988 |
Foreign Application Priority Data
| Current U.S. Class: |
514/231.5; 514/269; 514/275 |
| Intern'l Class: |
A61K 031/505 |
| Field of Search: |
514/275,231.5,269
|
References Cited
U.S. Patent Documents
| 4139619 | Feb., 1979 | Chidsey | 424/45.
|
| 4820512 | Apr., 1989 | Grollier | 424/70.
|
| Foreign Patent Documents |
| 905375 | Dec., 1986 | BE.
| |
Primary Examiner: Rizzo; Nicholas S.
Attorney, Agent or Firm: Fleit, Jacobson, Cohn, Price, Holman & Stern
Claims
There is claimed:
1. A combination of components, which is useful for the treatment of the
hair and scalp and is effective for inducing and stimulating hair growth
and for decreasing hair loss, comprising:
(a) a first component, (A), that contains an effective concentration of at
least one calcium antagonist in a physiologically acceptable medium; and
(b) a second component, (B), that contains, in a physiologically acceptable
medium, an effective concentration of at least one compound of formula
(I):
##STR6##
as well as acid addition salts thereof with physiologically acceptable
acids,
wherein:
R.sub.1 is a group having the formula
##STR7##
R.sub.3 and R.sub.4 are either selected from the group consisting of
hydrogen, lower alkyl, alkenyl, alkylaryl and cycloalkyl groups that
contain 4 to 6 carbon atoms, in which the alkyl portions are lower alkyl,
or R.sub.3 and R.sub.4, with the nitrogen to which they are each bound,
form a heterocyclic group, which is unsubstituted or is substituted on the
carbon atoms with one to three lower alkyl, hydroxy, or alkoxy groups, and
which is selected from the group consisting of aziridinyl, azetidinyl,
pyrrolidinylm, piperidinyl hyxahydroazepinyl, heptamethylenimino,
octamethyleneimino, morpholino and 4-(lower alkyl)piperazinyl;
R.sub.2 is selected from the group consisting of hydrogen, lower alkyl,
alkenyl, alkoxyalkyl, cycloalkyl groups that contain 4 to 6 carbon atoms,
aryl, alkylaryl, arylalkyl, alkylarylalkyl, alkoxyarylalkyl and
haloarylalkyl, in which the alkyl portions are lower alkyl radicals;
said components are intended for use as a composition comprising said
components or as separate components that are used either simultaneously,
successively or intermittently; and
each of said concentrations is effective for inducing and stimulating the
growth of hair and decreasing its loss when said components are used as
said combination.
2. The combination of claim 1, wherein said calcium antagonists are
selected from the group consisting of papaverine derivatives,
1,4-dihydropyridine derivatives, benzothiazepine derivatives,
cinnamyl-piperazine derivatives, nicergoline and bepridil.
3. The combination of claim 2, wherein said calcium antagonists are
selected from the group consisting of verapamil and gallopamil,
nifedipine, nicardipine, nimodipine, niludipine, felodipine,
nitrenedipine, nisoldipine, nivaldipine, isradipine, diltiazem,
cinnarizine and flunarizine.
4. The combination of claim 1, wherein R.sub.2 is hydrogen and R.sub.3 and
R.sub.4, with the nitrogen to which they are each bound, form a
piperidinyl heterocycle.
5. The combination of claim 4, wherein the compound of formula (I) is
6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine.
6. The combination of claim 1, wherein the concentration of the calcium
antagonist in said first component is between 0.01 and 10% by weight, and
the concentration of the compound of formula (I) is between 0.05 and 10%
by weight.
7. The combination of claim 1, wherein said first and second components are
present in a single composition and the concentration of the calcium
antagonist in said composition is between 0.01 and 5% by weight and the
concentration of the compound of formula (I) in said composition is
between 0.5 and 6% by weight.
8. The combination of claim 1, wherein said physiologically acceptable
media are water or a mixture of water and one or more organic solvents or
a mixture of cosmetically or pharmaceutically acceptable organic solvents.
9. The combination of claim 8, wherein at least one of said first and
second components contains a solvent selected from the group consisting of
C.sub.1 to C.sub.4 lower alcohols, alkyleneglycols and alkylethers of
monoand dialkyleneglycol.
10. The combination of claim 1, wherein at least one of said first and
second components is thickened by including thickening or gelling agents
in said medium.
11. The combination of claim 1, wherein at least one of said first and
second components also contains a cosmetically or pharmaceutically
acceptable additive selected from the group consisting of preservatives,
complexing agents, dyes, alkalizing or acidifying agents, anionic
surfactants, cationic surfactants, nonionic surfactants, amphoteric
surfactants, mixtures of anionic, cationic, nonionic or amphoteric
surfactants, anionic polymers, cationic polymers, nonionic polymers,
amphoteric polymers and mixtures of anionic, cationic, nonionic or
amphoteric polymers.
12. A method for cosmetically treating the hair or scalp, comprising
applying an effective amount of the combination of claim 1 to the hair or
scalp, wherein said amount is effective for said cosmetic treatment and
said components are mixed before use or applied either simultaneously,
successively or intermittently to the hair or scalp.
13. A multicompartment device, comprising component (A) in a first
compartment and component (B) in a second compartment, wherein:
(a) component (A) contains an effective concentration of at least one
calcium antagonist in a physiologically acceptable medium; and
(b) component (B) contains an effective concentration of at least one
pyrimidine derivative having a formula:
##STR8##
as well as acid addition salts thereof with physiologically acceptable
acids;
R.sub.1 is a group having the formula
##STR9##
R.sub.3 and R.sub.4 are either selected from the group consisting of
hydrogen, lower alkyl, alkenyl, alkylaryl and cacloalkyl groups that
contain 4 to 6 carbon atoms, in which the alkyl portions are lower alkyl,
or R.sub.3 and R.sub.4, with the nitrogen to which they are each bound,
form a heterocyclic group, which is unsubstituted or is substituted on the
carbon atoms with one to three lower alkyl, hydroxy, or alkoxy groups, and
which is selected from the group consisting of aziridinyl, azetidinyl,
pyrrolidinyl, piperidinyl, hyxahydroazepinyl, heptamethylenimino,
octamethyleneimino, morpholino and 4-(lower alkyl)piperazinyl;
R.sub.2 is selected from the group consisting of hydrogen, lower alkyl,
alkenyl, alkoxyalkyl, cycloalkyl groups that contain 4 to 6 carbon atoms,
aryl, alkylaryl, arylalkyl, alkylarylalkyl, alkoxyarylalkyl and
haloarylalkyl, in which the alkyl portions are lower alkyl radicals;
said components are intended for use as a composition comprising said
components or as separate components that are used either simultaneously,
successively or intermittently; and
each of said concentrations is effective for inducing and stimulating the
growth of hair and decreasing its loss when said components are used as
said combination.
14. A medicament for the therapeutic treatment of hair loss, comprising the
an effective amount of the combination of claim 1 and a carrier suitable
for topical application of said medicament to the hair or scalp.
15. A method for preparing the medicament of claim 14, comprising mixing
effective amounts of each of the components of said combination with said
carrier, wherein said amounts are effective for the therapeutic treatment
of hair loss.
16. A combination of components, which is useful for the treatment of the
hair and scalp and is effective for inducing and stimulating hair growth
and for decreasing hair loss, comprising:
(a) a first component, (A), that contains an effective concentration of at
least one benzothiazepine derivative in a physiologically acceptable
medium; and
(b) a second component, (B), that contains an effective concentration of at
least one compound of formula (I):
##STR10##
as well as acid addition salts thereof with physiologically acceptable
acids,
wherein:
R.sub.1 is a group having the formula
##STR11##
R.sub.3 and R.sub.4 are either selected from the group consisting of
hydrogen, lower alkyl, alkenyl, alkylaryl and cycloalkyl groups, or
R.sub.3 and R.sub.4, with the nitrogen to which they are each bound, form
a heterocyclic group, which is unsubstituted or is substituted on the
carbon atoms with one to three lower alkyl, hydroxy, or alkoxy groups, and
which is selected from the group consisting of aziridinyl, azatidinyl,
pyrrolidinyl, piperidinyl, hexahydroazapinyl, heptamethylenimino,
octamethyleneimino, morpholino and 4-(lower alkyl)piperazinyl;
R.sub.2 is selected from the group consisting of hydrogen, lower alkyl,
alkenyl, alkoxyalkyl, cycloalkyl, aryl, alkylaryl, arylalkyl,
alkylarylalkyl, alkoxyarylalkyl and haloarylalkyl,
said components are intended for use as a composition comprising said
components or as separate components that are used either simultaneously,
successively or intermittently; and
each of said concentrations is effective for inducing and stimulating the
growth of hair and decreasing its loss when said components are used as
said combination.
17. The combination of claim 16, wherein the benzothiazepine derivative is
diltiazem and the compound of formula (I) is
6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine.
18. The combination of claim 6, wherein the concentration of the calcium
antagonist in component (A) is between 0.01 and 5% by weight, and the
concentration of the compound of formula (I) in component (B) is between
0.05 and 5% by weight.
19. The combination of claim 18, wherein the concentration of said compound
of formula (I) is between 0.5 and 4% by weight.
20. The combination of claim 7, wherein the concentration of the calcium
antagonist in said composition is between 0.05 and 3% by weight, and the
concentration of the compound of formula (I) in said composition is
between 0.1 and 5% by weight.
21. The combination of claim 20, wherein the concentration of said compound
of formula (I) is between 0.5 and 2% 10 by weight.
Description
BACKGROUND OF THE INVENTION
Field of the Invention
The invention concerns a novel combination of a calcium antagonist and a
pyrimidine derivative intended to induce and stimulate hair growth, also a
method of treatment using said combination.
An individual has about 100 000 to 150 000 hairs on his head and normally
50 to 100 are lost daily. The number is maintained primarily because a
hair has a pilary life cycle comprising formation, growth and fall before
being replaced by a new hair appearing from the same follicle.
There are three phases in the pilary cycle: the anagenous, catagenous and
telogenous phases.
During the first, anagenous, phase the hair goes through a period of active
growth associated with intense metabolic activity in the root.
The second, catagenous, phase is transient and characterized by slowing of
mitotic activities. During this phase the hair undergoes involution, the
follicle atrophies and its dermal implantation appears increasingly
raised.
The final, telogenous, phase corresponds to the follicle's rest period and
the hair finally falls out, pushed out by a newly-formed anagenous hair.
This continuous physical renewal process evolves naturally during ageing
with the hair becoming finer and the cycles shorter.
Alopecia occurs when this physical renewal process is accelerated or
perturbed, ie the growth phases are shortened, the hair goes into the
telogenous phase earlier and more hair falls out. Successive growth cycles
result in finer and finer, shorter and shorter hair, gradually ending up
as unpigmented down. This phenomenon may result in baldness.
"Minoxidil" (6-amino-1,2,-dihydro,l-hydroxy-2-imino-4-piperidinopyrimidine)
has already been used in treating hair loss in topical compositions which
reduce or end the effects of alopecia, induce and stimulate hair growth
and reduce hair loss.
Orally or parenterally administered calcium antagonists are known in the
therapy and treatment of cardiovascular ailments.
It has now, surprisingly been discovered that combining calcium antagonists
(which in themselves neither induce or stimulate hair growth nor slow hair
loss) with certain pyrimidine derivatives produces the surprising effect
of improving the induction and stimulation of hair growth and ameliorating
the slowing of hair loss.
In particular, the combination begins to act more quickly than these
compositions in isolation. Because of the combination, a lower
concentration of the pyrimidine derivative can be employed.
The efficacity or speed of action of a composition for the treatment of
alopecia can be especially well determined using a trichogram and in
particular a phototrichogram which, inter alia, allows the percentage of
hair in the anagenous phase to be determined with respect to the hair in
the telogenous phase.
In particular, a combination according to the invention will increase this
percentage compared with that when the compositions are used separately.
One object of the invention is to provide a combination of a calcium
antagonist and a pyrimidine derivative intended to induce or stimulate
hair growth and reduce hair loss.
Another object of the invention is to provide a cosmetic and/or
pharmaceutical composition comprising this combination.
A further object of the invention is to provide a device having several
compartments containing said combination.
Further objects of the invention will become apparent from the following
description and examples.
SUMMARY OF THE INVENTION
A combination according to the invention intended to induce and stimulate
hair growth and reduce hair loss is primarily characterized in that it
comprises:
a) a first component comprising at least one calcium antagonist in a
physiologically acceptable medium; and
b) a second component containing, in a physiologically acceptable medium, a
pyrimidine derivative having formula:
##STR3##
wherein R.sub.1 represents the group
##STR4##
in which R.sub.3 and R.sub.4 are independent of each other and represent
hydrogen, an alkyl, alkenyl, alkylaryl or cycloalkyl group, or R.sub.3 and
R.sub.4 form a heterocycle with the nitrogen atom joined thereto, and
represent an aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl,
hexahydroazepinyl, heptamethyleneimine,
octamethyleneimine, morpholine or 4-alkylpiperazidinyl group, the
heterocyclic groups further being substitutable at the carbon atoms by one
to three low alkyl, hydroxy or alkoxy groups; and
R.sub.2 represents a hydrogen atom, an alkyl, alkenyl, alkylalkoxy,
cycloalkyl, aryl, alkylaryl, arylalkyl, alkylarylalkyl, alkoxyarylalkyl or
haloarylalkyl group, as well as the addition salts of physiologically
acceptable acids; in which combination said first and second components
form part of the same composition or are intended for separate use, either
simultaneously or in successive or separate stages.
More particularly, said calcium antagonist is selected from the group
comprising papaverine derivatives, 1,4-dihydropyridine derivatives,
benzothiazepine derivatives, cinnamypiperazine derivatives, nicergoline
and bepridil.
Particularly preferred papaverine derivatives are:
bis1,7-(3,4-dimethoxyphenyl)-5-methyl-1-isopropyl1-cyano-5-azaheptane
(verapamil) and its hydrochloride and
5[-methylamino-[2-(3,5-dimethoxyphenyl)ethyl]]-2-isopropyl-2-(3,4,5-trimet
hoxyphenyl) valeronitrile (gallopamil).
1,4-dihydropyridine derivatives are selected from the group comprising:
4-(2'-nitrophenyl)-2,6-dimethyl-3,5-dicarbomethoxy-1,4-dihydropyridine
(nifedipine);
4-(3'-nitrophenyl)-2,6-dimethyl-3-carbomethoxy-5-(methylbenzylamino)-carbo
xyethoxy-1,4-dihydropyridine )nicardipine) and its hydrochloride;
4-(3'-nitrophenyl-2,6-dimethyl-3-carbo-2-methoxyethoxy)-5-carboisopropoxy-
1,4-dihydropyridine (nimodipine);
4-(3'-nitrophenyl)-2,6-dimethyl-3,5-dicarbo-2-propoxyethoxy-1,4-dihydropyr
idine (niludipine);
4-(2'3'-dichlorophenyl)-2,6-dimethyl-3-carboethoxy-5-carbomethoxy-1,4-dihy
dropyridine (felodipine);
4-(3'-nitrophenyl)-2,6-dimethyl-3-carboethoxy-5-carbomethoxy
1,4-dihydropyridine (nitrendipine);
4-(3'nitrophenyl)-2-cyano-6-methyl-3-carbomethoxy-5-carbo-(1-methylethoxy)
-1,4-dihydropyridine (nilvadipine);
4-(4'-benzofurazanyl)-2,6-dimethyl-3-carbomethoxy-5-carbo-(1-methylethoxy)
-1,4dihydropyridine
(isradipine)-4-(2'-nitrophenyl)-2,6-dimethyl-3-carboisobutoxy-5-carbometho
xy-1,4dihydropyridine (nisoldipine).
Particularly preferred benzothiazepine derivatives are
3-acetyloxy-5-[2-(dimethylamino)ethyl]-2,3-dihydro-2-(4-methoxyphenyl)-1,5
-benzothiazepine-4 (5H)-one (diltiazem) and its hydrochloride.
Particularly preferred cinnamylpiperazines are
1-cinnamyl-4-diphenylmethylpiperazine (cinnarizine), its hydrochloride and
its clofibrate and 1-cinnamyl-4-di [(parafluorophenyl)methyl] piperazine
(flunarizine) and its hydrochloride.
A particularly preferred nicergoline is
(10-methoxy-1,6-dimethylergoline)-8- methanol 5-bromonicotinate.
A particularly preferred bepridil is 1-isobutoxy
2-pyrrolidino-3-N-benzylanilinopropane.
Most particularly preferred calcium antagonists are: verapamil, nifedipine,
nicardipine, diltiazem, cinnarizine and flunarizine.
In substances having formula (I), "alkyl or alkoxy" group preferably
defines a group containing one to four carbon atoms; "alkenyl" group
preferably defines a group containing two to five carbon atoms; "aryl"
group preferably defines a phenyl group and "cycloalkyl" group preferably
defines a group containing four to six carbon atoms.
Particularly preferred substances having formula (I) are those where R2
represents hydrogen and R.sub.1 represents the group:
##STR5##
where R.sub.3 and R.sub.4 represent a piperidinyl cycle, also their salts
such as the sulfate, for example.
A particularly preferred substance of this type is
6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine, known under
the trade name "Minoxidil".
The calcium antagonist is preferably present in the first component in a
proportion of between 0.01 and 10% by weight, preferably between 0.01 and
5% by weight and particularly between 0.1 and 3% by weight. The pyrimidine
derivative having formula (I) is preferably present in the second
component in a proportion of between 0.05 and 10% by weight, preferably
between 0.05 and 5% by weight, and particularly between 0.5 and 4% by
weight.
When the first and second components are used in a single composition, the
calcium antagonist is preferably present in a proportion of between 0.01
and 5% by weight and preferably between 0.05 and 3% by weight with respect
to the total composition weight; the pyrimidine derivative having formula
(I) is employed in a proportion of between 0.05 and 6% by weight,
preferably between 0.1 and 5% and particularly between 0.5 and 2% by
weight with respect to the total composition weight.
Physiologically acceptable media which could be employed include water,
water/solvent mixtures or mixtures of cosmetically or pharmaceutically
acceptable organic solvents.
More particularly, solvents such as the following may be used: C.sub.1 to
C.sub.4 low alcohols, for example ethanol, isopropanol, tert-butanol;
alkyleneglycols such as propyleneglycol; and alkylethers of mono- and
dialkyleneglycol, most particularly the monoethylether of ethyleneglycol,
the monomethylether of propyleneglycol and the monoethylether of
diethyleneglycol.
When used in an aqueous medium, these solvents are preferably present in
proportions of between 1 and 80% by weight with respect to the total
composition weight.
The physiologically acceptable media may be thickened if desired.
Thickening or gelling agents which are known in the art may be used,
particularly heterobiopolysaccharides such as xanthane gum or
scleroglucanes, cellulose derivatives and reticulated or unreticulated
acrylic polymers.
Thickeners are preferably present in proportions of between 0.1 and 5% by
weight, particularly between 0.4 and 3% by weight with respect to the
total weight of each component when they are used separately or with
respect to the total weight of a composition containing both the first and
second components.
Compositions constituted either by the first and second components
separately or both components together may contain any other additives
which are in general use in topical cosmetic or pharmaceutical
compositions. In particular, preservatives, complexing agents, dyes,
alkalizing or acidifying agents, surfactants, anionic, cationic, nonionic
and amphoteric agents or mixtures thereof, and anionic, cationic, nonionic
and amphoteric polymers or mixtures thereof may be employed.
Composition pH may vary between 4 and 9.
These compositions may also be packaged under pressure in an aerosol
device.
In the second component, pyrimidine derivatives having formula (I) may be
present either dissolved in the physiologically acceptable medium, or
entirely or partially in suspension in this medium, particularly as
particles having a granulometry below 80 microns, preferably below 20
microns and particularly below 5 microns.
A first embodiment of the invention consists in using the combination
defined above in a single composition containing the first and second
components.
A particularly preferred embodiment of the invention consists in storing
the first and second components in separate means and preparing the
composition containing the calcium antagonist and the pyrimidine
derivative having formula (I) extemporaneously immediately prior to
application.
Finally, a further embodiment consists in applying the first and second
components separately, either simultaneously or in successive or separate
stages.
A combination according to the invention may in this case be packaged as a
kit in a device having several compartments whose first compartment
contains the first component comprising the calcium antagonist and whose
second compartment contains the second component comprising the pyrimidine
derivative having formula (I). This device may further comprise mixing
means for preparing the composition just prior to application.
A treatment to induce and stimulate hair growth and reduce hair loss
consists principally in applying the combination defined above to the
areas of the scalp affected by alopecia, either using a single composition
or by applying the first and then the second component or vice-versa
successively or in separate stages.
A preferred method of application consists in applying 1 to 5 g of single
composition or of each of the first and second components to the area
affected by alopecia, once or twice a day, one to seven days a week for a
period of one to six months.
The treatment method has the characteristics of a therapeutic treatment in
that the inventive combination has a therapeutic action on the biological
mechanisms of the pilary cycle and its dysfunction.
An object of the invention is thus constituted by the use of a combination
which induces or stimulates hair growth and reduces hair loss.
The inventive method also has the characteristics of a cosmetic treatment
method in that it improves the hair or scalp.
EXAMPLES OF THE INVENTION
The following examples are intended to illustrate the invention without in
any way limiting its scope.
EXAMPLE 1
A lotion having the following composition was prepared:
______________________________________
verapamil hydrochloride
0.60 g
Minoxidil 1.00 g
propyleneglycol 20.00 g
ethanol 50.00 g
water qsp 100.00
g
______________________________________
EXAMPLE 2
A lotion having the following composition was prepared:
______________________________________
diltiazem hydrochloride
0.90 g
Minoxidil 1.00 g
ethanol 95.00 g
propyleneglycol qsp 100.00
g
______________________________________
EXAMPLE 3
A lotion having the following composition was prepared:
______________________________________
nifedipine 0.15 g
Minoxidil 1.00 g
propyleneglycol 20.00 g
ethanol 50.00 g
water qsp 100.00
g
______________________________________
EXAMPLE 4
The following first and second compositions (A) and (B) were packaged in
kit form:
______________________________________
Composition (A):
flunarizine hydrochloride
0.20 g
ethanol 95.00 g
propyleneglycol qsp 100.00
g
Composition (B):
Minoxidil 3.00 g
propylenegylcol 20.00 g
ethanol 50.00 g
water qsp 100.00
g
______________________________________
An extemporaneous mixture of compositions (A) and (B) was applied.
EXAMPLE 5
The following first and second compositions (A) and (B) were packaged in
kit form:
______________________________________
Composition (A):
nicardipine hydrochloride
0.60 g
propyleneglycol 20.00 g
ethanol 50.00 g
water qsp 100.00
g
Composition (B):
micronised Minoxidil (mean particle
2.00 g
size below 2 microns)
reticulated polyacrylic acid
1.00 g
M. Wt = 3 million, sold under the
trade name "CARBOPOL 934"
by GOODRICH
propyleneglycol 4.50 g
2-amino-2-methyl-1-propanol
qs pH = 7
preservative qs
water qsp 100.00
g
______________________________________
The compositions were applied in separate stages: composition (A) in the
morning and composition (B) in the evening.
EXAMPLE 6
The following first and second compositions (A) and (B) were packaged in
kit form:
______________________________________
Composition (A):
cinnarizine 0.50 g
ethanol 95.00 g
propyleneglycol qsp 100.00
g
Composition (B):
Minoxidil 2.00 g
ethanol 95.00 g
propyleneglycol qsp 100.00
g
______________________________________
The compositions were applied in separate daily stages: first day,
composition (A); second day, composition (B).
In each of examples 1 to 6, following daily application of the
composition(s) to areas of the scalp affected by alopecia for three months
a considerable improvement in the ratio anagenous/telogenous hair was
observed.
EXAMPLE 7
A lotion having the following composition was prepared:
______________________________________
diltiazem 3.00 g
Minoxidil 0.54 g
propyleneglycol 20.00 g
ethanol 50.00 g
water qsp 100.00
g
______________________________________
EXAMPLE 8
A lotion having the following composition was prepared:
______________________________________
cinnarizine 3.00 g
Minoxidil 0.54 g
propyleneglycol 20.00 g
ethanol 50.00 g
water qsp 100.00
g
______________________________________
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